Isoquinolinone derivatives, process for preparing the same, and their use as phosphodiesterase inhibitors

摘要

An isoquinolinone derivative of formula (I) wherein Ring A and Ring B are substituted or unsubstituted benzene, R<1> is (1) H, (2) substituted or unsubstituted lower alkyl, (3) substituted or unsubstituted cyclo-lower alkyl, (4) substituted or unsubstituted aryl, (5) substituted or unsubstituted heterocycle, or (6) amino optionally having one or two substitutents, R<2> is -COOR<3> or -CON(R<4>)(R<5>), R<3> is H or ester residue, and -N(R<4>)(R<5>) is substituted or unsubstituted nitrogen-containing aliphatic heterocycle or substituted or unsubstituted amino, provided that when R<1> is H or substituted or unsubstituted lower alkyl, then at least one of Ring A and Ring B is benzene being substituted by two or more lower alkoxy, or a pharmaceutically acceptable salt thereof, these compounds showing cGMP-specific PDE inhibitory activity, especially, selective phosphodiesterase V (PDEV) inhibitory activity, and hence, being useful for the prophylaxis or treatment of various diseases such as chronic heart failure, angina, pulmonary hypertension, erectile dysfunction, etc.